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. 2023 Sep 21;4(9):1345–1361. doi: 10.1038/s43018-023-00630-y

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© The Author(s) 2023, corrected publication 2023

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Extended Data Fig. 3 — (a) X-ray crystal structure shows that TAS compound 1 fits into a pocket surrounded by L730, G731, F735, V738 and L881. (b) View from the gatekeeper residue (V804) in the X-ray structure of the RET-TAS compound 1 complex. TAS Compound 1 is shown as a stick model in yellow. (c) Crystal structures of human RET complexed with TAS compound 1, selpercatinib or pralsetinib. In all three structures, RET showed the active conformation; DFG-in, αC helix-in, Activation Segment-out, and R spine-liner. Therefore, the three drugs can potentially be classified as type I inhibitors.